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free fatty acid receptor 1; G-protein coupled receptor 40 (FFAR1, GPR40)
Function:
- receptor for medium & long chain saturated fatty acids & unsaturated fatty acids
- binding of ligand increases intracellular Ca+2 concentration & amplifys glucose-stimulated insulin secretion
- activity is mediated by G proteins that activate phospholipase C
- seems to act through a Gq & Gi-mediated pathway
Structure:
- belongs to the G-protein coupled receptor 1 family
Compartment:
- cell membrane; multi-pass membrane protein
Expression:
- abundantly expressed in pancreatic beta cells
Pharmacology:
- TAK-875 is an experimental hypoglycemic agent for treatment of diabetes mellitus type 2 is an agonist of FFAR1
General
glycoprotein
phosphoprotein
G-protein coupled receptor; serpentine receptor
Properties
SIZE: entity length = 300 aa
MW = 31 kD
COMPARTMENT: cellular membrane
MOTIF: exoplasmic domain {1-10}
transmembrane domain {11-31}
cytoplasmic loop {32-42}
transmembrane domain {43-63}
MOTIF: Tyr phosphorylation site {Y44}
exoplasmic loop {64-81}
transmembrane domain {82-102}
cytoplasmic loop {103-123}
transmembrane domain {124-144}
exoplasmic loop {145-178}
MOTIF: N-glycosylation site {N155}
transmembrane domain {179-197}
cytoplasmic loop {198-221}
transmembrane domain {222-242}
exoplasmic loop {243-258}
transmembrane domain {259-279}
cytoplasmic domain {280-300}
Database Correlations
OMIM 603820
UniProt O14842
Pfam PF00001
Entrez Gene 2864
Kegg hsa:2864
References
UniProt :accession O14842